Bicalutamide


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Palliation of advanced prostate cancer 50 mg once daily, w/ gonadotropin-releasing hormone (GnRH) agonist or surgical castration. Monotherapy or adjuvant therapy to surgery or radiotherapy in locally advanced prostatic cancer 150 mg once daily.
Dosage Details
Oral
Palliative treatment of advanced prostate cancer
Adult: 50 mg once daily. May be started at the same time or at least 3 days before therapy w/ gonadotropin-releasing hormone (GnRH) agonist; it may also be used in combination w/ surgical castration, starting on the same day as surgery.

Oral
Monotherapy or adjuvant therapy to surgery or radiotherapy in locally advanced prostatic cancer
Adult: 150 mg once daily.
Administration
May be taken with or without food.
Contraindications
Females, childn. Pregnancy and lactation. Concomitant use of terfenadine, astemizole or cisapride.
Special Precautions
Patient w/ decreased bone density, history of or risk factors for QT prolongation, diabetes, Moderate to severe hepatic and severe renal impairment (CrCl <30 mL/min).
Adverse Reactions
Anaemia; angioedema, urticaria; decreased appetite, DM, wt gain, dehydration, gout; decreased libido, depression, anxiety, hypertonia, confusion, neuropathy, nervousness, dizziness, somnolence; hot flush; abdominal pain, constipation, nausea, dyspepsia, flatulence, anorexia, rectal haemorrhage, dry mouth, melaena; hepatotoxicity, jaundice, hypertransaminasaemia; alopecia, hirsutism, dry skin, pruritus/rash, photosensitivity; haematuria, dysuria, urinary retention, impaired urination, urinary frequency; gynaecomastia, breast tenderness, erectile dysfunction; asthenia, oedema, chest pain, neck pain, fever, sepsis, chills, neoplasm; cough, pharyngitis, bronchitis, pneumonia, rhinitis.
Potentially Fatal: MI, cardiac failure, QT prolongation, interstitial lung disease, hepatic failure.
Patient Counseling Information
This drug may cause somnolence, if affected, do not drive or operate machinery.
MonitoringParameters
Perform LFT at baseline and regularly (particularly during the 1st 6 mth of therapy), then periodically thereafter. Monitor CBC, ECG, echocardiograms, serum testosterones, LH and serum prostate specific antigen.
Drug Interactions
May induce torsade de pointes or QT prolongation if co-administered w/ class IA (e.g. quinidine) or class III (e.g. amiodarone) antiarrhythmic agents, methadone, antipsychotics, moxifloxacin. Enhanced anticoagulant effect of warfarin. Increased adverse effects when used w/ drugs that may inhibit oxidation (e.g. cimetidine, ketoconazole). May increase serum levels of ciclosporin and Ca channel blockers.
Potentially Fatal: Additive effect in prolonging QT interval w/ terfenadine, astemizole and cisapride.
Food Interaction
Alcohol may exacerbate facial flushing, avoid use.
Action
Description: Bicalutamide competitively blocks the binding of androgen receptors in target tissues, resulting in growth arrest or transient tumour regression through inhibition of androgen-dependent DNA and protein synthesis.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Time to peak plasma concentration: Approx 31 hr (R-enantiomer).
Distribution: Plasma protein binding: Approx 96%.
Metabolism: Metabolised extensively in the liver via glucuronidation and oxidation of the R-enantiomer (active); the S-enantiomer is inactive.
Excretion: Via urine and faeces, as metabolites. Elimination half-life: Approx 6 days (R-enantiomer).
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store between 20-25°C.
ATC Classification
L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
Disclaimer: This information is independently developed by MIMS based on Bicalutamide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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